DETAILED ACTION
Claims 1-22 are currently pending in the instant application. Claims 2-11, 16, and 17 are rejected. Claims 1-17, 21 and 22 are objected. Claims 18-20 are withdrawn from consideration as being for non-elected subject matter.
Notice of Pre-AIA or AIA Status
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
Election/Restrictions
Applicant’s election without traverse of Group I, claims 1-17 in the reply filed on 4 September 2025 is acknowledged. Additionally, Applicant’s election of the species
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in the reply filed 15 October 2025 is acknowledged.
According to MPEP 803.02, the examiner has determined whether the elected species is allowable. Applicants’ elected species appears allowable. Therefore, the search and examination has been extended to the entirety of the compound of the formula I, its tautomer, mesomer, racemate, enantiomer, diastereoisomer, or mixtures thereof, and a pharmaceutically acceptable hydrate, solvate, or a salt thereof which also appears allowable and further to the compound:
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which is not allowable and is an isomer of the elected species.
Claims 1-17, 21 and 22 have been examined to the extent that they are readable on the elected embodiment, the elected species and the above mentioned compounds.
Specification
The specification is objected to as failing to provide proper antecedent basis for the claimed subject matter. See 37 CFR 1.75(d)(1) and MPEP § 608.01(o). Correction of the following is required: Specifically, claim 1 to formula I:
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defines A2 as:
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wherein Z1 and Z2 are independently 1-5. There is no antecedent basis in the specification for the definition of R12.
Applicant’s instant specification provides the formula I:
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on page 4 wherein A2 is defined as:
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wherein R12 is defined as:
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which is broader than the instant claimed subject matter in regards to A2. Page 9 provides the sub formula:
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, wherein R19 can be
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which is a more narrow and different scope of the instant claimed subject matter, see for example wherein the sub formula do not include A3 being N when A1 is -CR1. As seen on pages 4 and 9 of the specification, there is no antecedent basis for the definition of R12 as
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on the formula I:
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Claim Objections
Claims 1-17, 21 and 22 are objected to because of the following informalities:
Claims 1-17, 21 and 22 have a multitude of grammatical errors such as grammar or typographical errors. Additionally, the claims are not written uniformly as some claims are singular where others are plural, some groups include the word “group” where others do not, some substituents are plural when others are singular, some claims use unsubstituted while others use non-substituted, or the claims use unnecessary terminology such as “stated in”, “shown in”, and “characterized.” For the sake of clarity, consistency and for proper Markush language, the examiner has provided a set of claims attached to the instant office action (Appendix A) that is a suggestion on how to amend the claim set to overcome the various objections to the claims. Appropriate correction is required.
For example,
Claim 1 has “A1” in the structure of formula I, but defines “A1”. The same applies for A2, and A3. R12 is mentioned both as “R12” and “R12”
Claim 3 the number of carbons, such as in C1-C3 should be subscript. Additionally, as claim 1 uses the terminology of “unsubstituted”, instances of “non substituted” should be changed to “unsubstituted.” Claim 3 has a capital letter in “Wherein” in the middle of the claim which should be lower case.
Claim 4 the number of carbons, such as in C1-C6 should be subscript. Additionally, as claim 1 uses the terminology of “unsubstituted”, instances of “non substituted” should be changed to “unsubstituted.” Claim 4 has a capital letter in “Wherein” in the middle of the claim which should be lower case. Claim 4 has an extra comma. An instance of “halogen” is spelled incorrectly. Lastly, claim 4 is written as plural when all other claims are written as singular.
Claim 5 the number of carbons, such as in C1-C6 should be subscript. Additionally, as claim 1 uses the terminology of “unsubstituted”, instances of “non substituted” should be changed to “unsubstituted.” Lastly some ring groups are provided, such as 2- and 7-membered instead of 2- to 7-membered.
Claim 6 the number of carbons, such as in C1-C3 should be subscript. Additionally, as claim 1 uses the terminology of “unsubstituted”, instances of “non substituted” should be changed to “unsubstituted.”
Claim 7 as claim 1 uses the terminology of “unsubstituted”, instances of “non substituted” should be changed to “unsubstituted.”
Claim 8-10 the number of carbons, such as in C1-C3 and C1-C6 should be subscript. Additionally, as claim 1 uses the terminology of “unsubstituted”, instances of “non substituted” should be changed to “unsubstituted.”
Claim 14 is written as plural when all other claims are written as singular. Claim 14 needs a space between “clam1” to read “claim 1”. Additionally, the number of carbons, such as in C1-C3 should be subscript.
Claim 15 provides a structure wherein the text is too small and illegible, the claims must have text written plainly and legibly in a nonscript type font (e.g., Arial, Times Roman, or Courier, preferably a font size of 12) lettering style having capital letters which should be at least 0.3175 cm. (0.125 inch) high, but may be no smaller than 0.21 cm. (0.08 inch) high (e.g., a font size of 6) in portrait orientation and presented in a form having sufficient clarity and contrast between the paper and the writing thereon to permit the direct reproduction of readily legible copies in any number by use of photographic, electrostatic, photo-offset, and microfilming processes and electronic capture by use of digital imaging and optical character recognition; and only a single column of text. See 37 CFR 1.52(a) and (b). The structure provided in claim 15:
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is in a font size that is too small to have sufficient clarity.
Claim 17 has extra space after the second comma in line 2.
Claims 21 and 22 are new claims. New claims do not require underlining. Additionally, as only one structure is presented, “selected from” is unnecessary.
Claim Rejections - 35 USC § 112
The following is a quotation of the first paragraph of 35 U.S.C. 112(a):
(a) IN GENERAL.—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention.
The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. 112:
The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor of carrying out his invention.
Claims 2-11 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, because the specification, while being enabling for the compound of claim 1 or a tautomer, a mesomere, a racemate, an enantiomer, a diastereoisomer or a mixture thereof, or a pharmaceutically acceptable hydrate, solvate, or salt thereof, does not reasonably provide enablement for any isomer thereof. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make or use the invention commensurate in scope with these claims.
In In re Wands, 8 USPQ2d 1400 (1988), factors to be considered in determining whether a disclosure meets the enablement requirement of 35 U.S.C. § 112, first paragraph, have been described. They are:
1. the nature of the invention,
2. the state of the prior art,
3. the predictability or lack thereof in the art,
4. the amount of direction or guidance present,
5. the presence or absence of working examples,
6. the breadth of the claims,
7. the quantity of experimentation needed, and
8. the level of the skill in the art.
The nature of the invention
The nature of the invention is products of the formula I, II”, IV and IV” including isomers, tautomers, mesomers, racemates, enantiomers, diastereoisomers or the mixtures, and pharmaceutically acceptable hydrates, solvates or salts.
The state of the prior art and the predictability or lack thereof in the art
The state of the prior art is that an isomer is any compound having the same composition, including constitutional isomers, which are compounds whose atoms are connected differently. Constitutional isomers can contain different functional groups in varying positions.
The amount of direction or guidance present and the presence or absence of working examples
The only direction or guidance present in the instant specification is for tautomers, mesomers, racemates, enantiomers and diastereoisomers, see pages 15 and 16 of the specification.
There is no data present in the instant specification for the preparation or utility of constitutional isomers.
The breadth of the claims
The instant breadth of the rejected claims is broader than the disclosure, specifically, the instant claims include any isomer, i.e. any compound with the same number of each atom.
The quantity or experimentation needed and the level of skill in the art
While the level of the skill in the pharmaceutical arts is high, it would require undue experimentation of one of ordinary skill in the art to prepare any isomer as instantly claimed since an isomer of the compounds need only have the same composition of atoms, not necessarily the same order of atoms and can have varying functional groups in varying positions. Therefore, the claims lack enablement for all isomers.
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claim 17 is rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being indefinite for failing to particularly point out and distinctly claim the subject matter which the inventor or a joint inventor (or for applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention.
Claim 17 recites the limitation "for use in the Nav1.8 inhibitor" in reference to the compounds of claim 1. There is insufficient antecedent basis for this limitation in the claim as there is no “a Nav1.8 inhibitor” in claim 1. It is suggested that claim 17 be canceled.
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claims 16 and 17 are rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends. Specifically, claims 16 and 17 are dependent upon claim 1 which claims compounds of the formula I or a tautomer, a mesomere, a racemate, an enantiomer, a diastereoisomer or a mixture thereof, or a pharmaceutically acceptable hydrate, solvate, or salt thereof. Instant claims 16 and 17 are claiming a pharmaceutical composition comprising the compound of claim 1 (claim 16) and a compound of claim 1 with an intended use (claim 17) which includes the compound or their stereoisomers, solvates, hydrates, and pharmaceutically acceptable salts or co-crystals. Claim 1 does not have co-crystals of the compound of the formula I. Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements. It is suggested that “co-crystals” be deleted from claims 16 and 17.
Claim Rejections - 35 USC § 102
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
The following is a quotation of the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention.
Claim(s) 2-11 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Kuramoto et al. J. Med. Chem, 2003, 46, 1905-1917.
Kuramoto et al discloses the compound 12c in Scheme 3 on page 1906:
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. The compound 12c is
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which has the molecular formula C23H19ClF4N2O5. Applicant’s elected species
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has the molecular formula C23H19ClF4N2O5, The compound 12c corresponds to a constitutional isomer of the elected species which has a molecular formula C23H19ClF4N2O5. The instant claims 2-11 claim isomers of the formula II:
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and IV”:
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which includes constitutional isomers of the elected species.
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to REBECCA L ANDERSON whose telephone number is (571)272-0696. The examiner can normally be reached Monday-Friday from 6am-2pm.
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Andrew Kosar can be reached at 571-272-0913. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/REBECCA L ANDERSON/Primary Examiner, Art Unit 1626 ____________________ 12 February 2026
Rebecca Anderson
Primary Examiner
Art Unit 1626, Group 1620
Technology Center 1600
Appendix A
Suggested Claim Set:
A compound of formula I or a tautomer, a mesomere, a racemate, an enantiomer, a diastereoisomer or a mixture thereof, or a pharmaceutically acceptable hydrate, solvate, or salt thereof:
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wherein,
A1 and A3 are independently CR1 or N;
A2 is OR12; z is 0;R12 is
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or
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R1, R2, and R3 are independently selected from the group consisting of hydrogen, halogen, hydroxyl, cyano, amino, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted amide, ester, acyl, carboxyl, sulfonyl, sulfonamido, boronic acid, boronic acid ester, phosphoryl, substituted or unsubstituted alkenyl group, and substituted or unsubstituted alkynyl group, wherein a substituent on R1, R2, and R3 is selected from the group consisting of deuterium, halogen, hydroxyl, amino, alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, cyano, ester, acyl, carboxyl, amido, aryl, heteroaryl, sulfonyl, and sulfonamido;
n is 0, 1, 2, 3, or 4;
m is 0, 1, 2, 3, 4, or 5;
R13 and R14 are independently selected from the group consisting of hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, and substituted or unsubstituted heteroaryl; and
Z1 and Z2 are independently 1-5.
The compound of claim 1 or the tautomer, mesomere, racemate, enantiomer, diastereoisomer or the mixture thereof, or the pharmaceutically acceptable hydrate, solvate, or salt thereof of formula II or II”:
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wherein, n is 0, 1, or 2 and m is 0, 1, or 2.
The compound of claim 2 or the tautomer, mesomere, racemate, enantiomer, diastereoisomer or the mixture thereof, or the pharmaceutically acceptable hydrate, solvate, or salt thereof of formula IV or IV”:
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wherein,
A₁ is N or CR₁;
R₁ is selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C1 to C3 alkyl, and substituted or unsubstituted 2- to 4- membered heteroalkyl, wherein a substituent on R1 is selected from the group consisting of halogen, hydroxyl, amino, C1 to C3 alkyl, 2- to 4- membered heteroalkyl, and acyl;
R19 is
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or
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;
Z₁ and Z₂ are independently 1-5;
R₁₃ and R₁₄ are independently hydrogen or
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R6, R₇, R₈, and R₉ are independently selected from the group consisting of hydrogen, halogen, hydroxyl, cyano, amino, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, ester, acyl, carboxyl, acylamino, sulfonyl, sulfonamido, boronic acid, boronic acid ester, phosphoryl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl, wherein a substituent on R6, R7, R8 and R9 is selected from the group consisting of deuterium, halogen, hydroxyl, amino, alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, cyano, ester, acyl, carboxyl, amide, aryl, heteroaryl, sulfonyl, and sulfonamido.
4. The compound of claim 3 wherein R6 and R7 are independently selected from the group consisting of hydrogen, halogen, hydroxyl, cyano, amino, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, ester, acyl, carboxyl, acylamino, sulfonyl, sulfonamido, boronic acid, boronic acid ester, phosphoryl, and substituted or unsubstituted alkenyl, wherein a substituent on R6 and R7 is selected from the group consisting of halogen, hydroxyl, amino, C1 to C6 alkyl, 3- to 6-membered cycloalkyl, 2- to 7-membered heteroalkyl, 3- to 6-membered heterocycloalkyl, cyano, ester, acyl, amido, aryl, heteroaryl, sulfonyl, and sulfonamido; and R8 and R9 are independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, hydroxyl, cyano, amino, ester, acyl, amido, and sulfonyl, wherein a substituent on R8 and R9 is selected from the group consisting of deuterium, alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, halogen, hydroxyl, cyano, amino, acylamino, and sulfonyl.
5. The compound of claim 3 wherein R6 and R7 are independently selected from the group consisting of hydrogen, halogen, hydroxyl, cyano, amino, substituted or unsubstituted C1 to C6 alkyl, substituted or unsubstituted 3- to 10-membered cycloalkyl, substituted or unsubstituted 2- to 7-membered heteroalkyl, substituted or unsubstituted 3- to 10-membered heterocycloalkyl, ester, acyl, phosphoryl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl, wherein a substituent on R6 and R7 is selected from the group consisting of halogen, hydroxyl, amino, C1 to C6 alkyl, 2- to 7-membered heteroalkyl, cyano, ester, acyl, amido, aryl, heteroaryl, sulfonyl, and sulfonamido; and R8 and R9 are independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted heterocycloalkyl, wherein a substituent on R8 and R9 is selected from the group consisting of deuterium, C1 to C6 alkyl, 2- to 7-membered heteroalkyl, 3- to 6-membered cycloalkyl, 3- to 6-membered heterocycloalkyl, halogen, hydroxyl, and acylamino group.
6. The compound of claim 3 wherein R6 and R7 are independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C1 to C3 alkyl, and substituted or unsubstituted cyclopropyl, and wherein R6 and R7 are not simultaneously hydrogen.
7. The compound of claim 3 wherein R6 and R7 are independently selected from the group consisting of hydrogen, halogen, trifluoromethyl, and substituted or unsubstituted cyclopropyl.
8. The compound of claim 3 wherein R8 and R9 are independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C1 to C6 alkyl, and substituted or unsubstituted C1 to C6 alkoxy, and wherein a substituent is selected from deuterium, halogen, C1 to C6 alkyl, 2- to 7-membered heteroalkyl, 3- to 6-membered cycloalkyl, 3- to 6-membered heterocycloalkyl, hydroxyl, and amide.
9. The compound of claim 3 wherein R8 is selected from the group consisting of halogen, substituted or unsubstituted C1 to C3 alkyl, and substituted or unsubstituted C1 to C3 alkoxy; and R9 is selected from the group consisting of halogen, methyl, trifluoromethyl, and substituted or unsubstituted alkoxy.
10. The compound of claim 3 wherein R8 is substituted or unsubstituted C1 to C3 alkyl; and R9 is selected from the group consisting of F, Cl, Br, methyl, trifluoromethyl, methoxy, and trifluoromethoxy.
11. The compound of claim 3 wherein R8 is methyl and R9 is F.
12. The compound of claim 1 wherein R1 is hydrogen or halogen.
13. The compound of claim 1 wherein R1 is H or F.
14. The compound of claim 1 wherein halogen is selected from the group consisting of F, Cl, and Br; substituted or unsubstituted C1 to C3 alkyl is methyl or trifluoromethyl; and the substituted or unsubstituted C1 to C3 alkoxy is methoxy or trifluoromethoxy.
15. A compound of formula
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or an enantiomer thereof.
16. A pharmaceutical composition comprising, as the active ingredient, the compound of claim 1 or the tautomer, mesomere, racemate, enantiomer, diastereoisomer or the mixture thereof, or the pharmaceutically acceptable hydrate, solvate, or salt thereof.
17. (canceled)
18. (canceled)
19. (canceled)
20. (canceled)
21. The compound of claim 15 wherein the compound is:
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.
22. The compound of claim 15 wherein the compound is:
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.